Crystalline form of sulfonamide derivative and preparation method therefor

EP4663635A4Pending Publication Date: 2026-06-24JIANGSU HENGRUI MEDICINE CO LTD +1
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Patent Information

Authority / Receiving Office
EP · EP
Patent Type
Applications
Current Assignee / Owner
JIANGSU HENGRUI MEDICINE CO LTD
Filing Date
2024-02-07
Publication Date
2026-06-24

AI Technical Summary

Technical Problem

Existing crystal forms of the sulfonamide derivative N-(5-((1H-pyrazol-1-yl)methyl)-3,4-dihydro-2H-benzopyran[8,7-d]isoxazol-9-yl)-2,6-dimethoxybenzenesulfonamide exhibit poor stability and agglomeration, posing challenges in production and storage, and require improved polymorphs for better clinical efficacy.

Method used

Development of six distinct crystal forms (A, B, C, D, E, F, G, and H) characterized by specific X-ray powder diffraction patterns, each prepared through various solvent-based crystallization methods, including trituration, stirring, and antisolvent crystallization, to enhance stability and clinical prospects.

Benefits of technology

The new crystal forms exhibit improved stability and flowability, addressing the issues of agglomeration and enhancing the drug's suitability for pharmaceutical applications, particularly in the treatment of cancers such as breast, ovarian, pancreatic, and lung cancer.

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Abstract

The present disclosure relates to a crystalline form of a sulfonamide derivative and a preparation method therefor. Specifically, the present disclosure provides a new crystalline form of a compound as represented by formula (1) and a preparation method therefor.
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